Pharmaceutical gastro-retentive solid oral dosage form of nilotinib

Patent metadata

Field	Value
Publication number	US-9682081-B2
Application number	US-201414787167-A
Country	US
Kind code	B2
Filing date	Apr 25, 2014
Priority date	Apr 25, 2013
Publication date	Jun 20, 2017
Grant date	Jun 20, 2017

Abstract

The present invention relates to a pharmaceutical gastro-retentive solid oral dosage form comprising nilotinib as the active ingredient. The invention is further related to methods of preparing said dosage form.

First claim

We claim:

1. A gastro-retentive tablet which comprises nilotinib or a salt thereof, at least one rate-controlling polymer which is a swelling agent, and other pharmaceutically acceptable excipients wherein the gastroretentive action of the tablet is based on swelling mechanism.

2. The gastro-retentive tablet of claim 1 , wherein the tablet further comprises an acidifying agent.

3. The gastro-retentive tablet of claim 1 , wherein the tablet is administered once daily or twice daily.

4. The gastro-retentive tablet of claim 1 , wherein the other pharmaceutically acceptable excipients are selected from diluents, matrix forming agents, disintegrants, binding agents, gas-generating agents, semi-permeable film-forming agents, glidants, and lubricants.

5. The gastro-retentive tablet of claim 4 , wherein the gas generating agent is selected from alkali metal carbonates and bicarbonates.

6. The gastro-retentive tablet of claim 5 , wherein the tablet containing the gas generating agent is uncoated.

7. The gastro-retentive tablet of claim 5 , wherein the gastro-retentive action of the solid dosage form is based on the mechanism of floatation.

8. A gastro-retentive tablet which comprises nilotinib or a salt thereof, at least one rate-controlling polymer, one or more osmogen agents, and other pharmaceutically acceptable excipients wherein the tablet is coated with a semi-permeable film and at least one hole or opening through the semi-permeable film for drug release.

9. A gastro-retentive tablet which comprises nilotinib or a salt thereof, at least one rate-controlling polymer, one or more osmogen agents, and other pharmaceutically acceptable excipients wherein the tablet is coated with a semi-permeable film comprising a film forming agent and a pore forming agent.

10. A gastro-retentive capsule comprising nilotinib and a diluent in the form of a powder, granules, or minitablet in the capsule wherein the capsule has an outer coating in the form of a semi-permeable film comprising a film forming agent and a pore forming agent and the capsule does not disintegrate until the drug is released.

Assignees

• Sun Pharmaceutical Ind Ltd

Inventors

• Fanda Anuj Kumar
• Sharma Ravish
• Vivek Kumaravel
• Khurana Lalit Kumar
• Ahmad Shavej
• Singh Romi Barat
• Singla Ajay Kumar

Classifications

• A61K9/0004

  Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas · CPC title

• A61K9/4891

  Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004) · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/506 Primary

  not condensed and containing further heterocyclic rings · CPC title

• A61K9/0065

  Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus · CPC title